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Article

Engaging an engineered PARP-2 catalytic domain mutant to solve the complex structures harboring approved drugs for structure analyses.

Bioorganic chemistry - 15 Jun 2025

Wang Xiaoyu, Zhou Jie, Xu Bailing

Abstract excerpt

The PARP-1/2 inhibitors have been approved for the treatment of cancers by modulating the enzymatic activity and/or the trapping ability for damaged DNA of PARP-1 and/or PARP-2, and the selective PARP-1 inhibitors are now attracting considerable attention with an aim to search for drug candidates with an improved safety. Exploring the structural basis of the selectivity and trapping capability of known PARP-1/2...

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Identifiers

PMID: 40228437
DOI: 10.1016/j.bioorg.2025.108471

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ASL

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